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Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring
- Source :
- Scopus-Elsevier
-
Abstract
- "A series of new histone deacetylase inhibitors were designed and synthesized based on hybridization between SAHA or oxamflatin and 5-phenyl-1,4-benzodiazepines. The compounds were tested for their enzyme inhibitory activity on HeLa nuclear extracts, and on human recombinant HDAC1 and HDAC6. Antiproliferative activity was tested on different cancer cells types, while proapoptotic activity was primarily tested on NB4 cells. The compounds showed IC50 values similar to those of SAHA. Compound (S)-8 displayed interesting activity against hematological and solid malignancies."
- Subjects :
- Antineoplastic Agents
Chemistry Techniques, Synthetic
Pharmacology
Histone Deacetylases
law.invention
HeLa
Benzodiazepines
Structure-Activity Relationship
law
HDAC
Cell Line, Tumor
Drug Discovery
Humans
Cancer
Cell Proliferation
biology
Chemistry
Organic Chemistry
Stereoisomerism
General Medicine
HDAC6
biology.organism_classification
HDAC1
Oxamflatin
Histone Deacetylase Inhibitors
Biochemistry
Solubility
Apoptosis
Drug Design
Cancer cell
Recombinant DNA
Epigenetics
Histone deacetylase
Subjects
Details
- Database :
- OpenAIRE
- Journal :
- Scopus-Elsevier
- Accession number :
- edsair.doi.dedup.....bbb3ae7b58e96c3db1d3be00fcbfcc57